2. Academic Validation
  3. Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity

Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity

  • Bioorg Med Chem Lett. 2008 Mar 1;18(5):1588-91. doi: 10.1016/j.bmcl.2008.01.072.
Hideyuki Onodera 1,  Masami Kaneko,  Yuichi Takahashi,  Yumiko Uochi,  Jun Funahashi,  Takayuki Nakashima,  Shiro Soga,  Makoto Suzuki,  Shunichi Ikeda,  Yoshinori Yamashita,  Endang S Rahayu,  Yutaka Kanda,  Michio Ichimura
Affiliations

Affiliation

  • 1 BioFrontier Laboratories, Kyowa Hakko Kogyo Co., Ltd., 3-6-6 Asahi-machi, Machida-shi, Tokyo 194-8533, Japan.
PMID: 18243703 DOI: 10.1016/j.bmcl.2008.01.072
Abstract

HSP90 is an attractive chemotherapeutic target because it is essential to maturation of multiple oncogenes. We describe the conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin isolated from Streptomyces sp. Their native free structures are similar to the active form of geldanamycin bound to HSP90 protein. Their conformational character is a probable reason for their high-affinity binding. Lack of toxic benzoquinone in EH21A1-A4 also adds to their potential as lead compounds for anti-tumor drugs.

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